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胺化作用

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According to Griess reaction, diazonium-salts formed from aromatic amines such as sulfonamides etc., react with NaNO_2 in acid medium and may be coupled with α-naphthylamine or diphenylamine to produce red colored compounds.

一按Griess反应芳香族胺类的重氮化鹽,如对氨基苯磺醯胺类药物等,在酸性溶液中皆能与α-萘胺或二苯胺分别偶合成偶氮色素而显紅色,过多之亞硝酸可与氮色素再作用使紅色消失而呈棕黄色。

The glutamine synthetase produced by the engineering bacteria can specially act on NH4 and aminoglutaric acid, the durability to the high concentration ammonium ion has been distinctively improved because of the dissolution of adenosine acylation modification, the major bottleneck of glutamine with enzymatical production has been solved, and the concentration of the obtained glutamine can reach 47.6g/L.

本发明工程菌产的谷氨酰胺合成酶可专一性的作用于NH 4 和谷氨酸,且因解除了腺苷酰化修饰作用对高浓度铵离子的耐受能力显著提高,解决了酶法生产谷氨酰胺的重要瓶颈,生成的谷氨酰胺的浓度最高达到47.6g/L。

Firstly, 3-ethylthiobutanal was prepared from crotonaldehyde reacting with ethanehiol in triethylamine with high yield. Secondly, methyl acetoacetate was converted to 6-ethylthiohept-3-en-2-one by three steps via hydrolysis, condensation with 3-ethyltio-butanal and dehydration, then 6-ethylthiohept-3-en-2-one was cycloco ndensed with dimethyl malonate by Michael addition and Claisen condensation, followed by saponification and decarboxylation to give the intermediate of 5-(2-ethylthiopropyl)-cyclohexane-1,3-dione.

首先,以巴豆醛与乙硫醇为原料,在三乙胺的催化作用下高收率制得3-乙硫基丁醛;然后从乙酰乙酸甲酯出发,通过碱水解、与3-乙硫基丁醛缩合、脱水三步反应合成6-乙硫基-3-烯-2-庚酮,接着6-乙硫基-3-烯-2-庚酮与丙二酸二甲酯通过Michael加成和Claisen缩合成环,再通过皂化和脱羧反应生成中间体5-[2-丙基]-1,3-环己二酮;再与丙酸酐反应丙酰化,最后与0-3-氯-2-丙烯基羟胺肟化,得到目标化合物烯草酮。

Tetrachloroterephthalic acid was prepared by chlorinating terephthalic acid, oleumsolvent and iodine catalyst. Tetrachloroterephthalic acid was acylated by sulphurous oxychloride in the presence of DMF to form tetrachloroterephthaloyl chloride. The acyl chloride product was fluorinated by potassium fluoride and esterified by methanol to synthesize dimethyl tetrafluoroterephthalate. The ester was reduced with potassium borohydride and lithium chloride to give tetrafluoroterephthalyl alcohol. The above product was bromated in the hydrobromic acid to obtain 4-bromomethyl-2,3,5,6-tetrafluoro-benzene methanol. 4-Methyl-2,3,5,-6-tetrafluorobenzene ethanol was obtained by reducing the bromide with magnesium. In the exist of DCC and DMAP, tefluthrin was got by the condensation reaction between 4-methyl-2,3,5,6-tetrafluoro-benzene methanol and-(1RS,3RS)- 3-(2- chloro-3,3,3-trifluoro-1-propenyl)-2,2-dimethyl cycolpropanecar-boxylate acid.

对苯二甲酸与氯气在碘存在下以发烟硫酸为溶剂进行氯化制备四氯对苯二甲酸;再以DMF为催化剂与二氯亚砜反应生成四氯对苯二甲酰氯;以氟化钾为氟化剂,环丁砜为溶剂置换氟化,再与甲醇酯化得到四氟对苯二甲酸甲酯;以KBH4-LiCl为还原剂二甲醚为溶剂反应制得四氟对苯二甲基苄醇;以氯苯为溶剂在溴化氢溶液中溴化得到溴化产物;在乙醇溶液中经镁粉还原得到4-甲基-2,3,5,6-四氟苄醇;甲基苄醇与功夫酸在催化剂二环己基碳二亚胺和4-二甲氨基吡啶作用下缩合得到七氟菊酯,总收率达43.6%。

Pharmacological results also indicated that the carbonyl and imino of Z-47 are important to its marked antiinflammatory and analgesic activity. The activity will be reduced or abolished with Z-47 converted to oximes or/and acetamides.

药理结果还表明,Z-47结构中的羰基和仲胺基对Z-47的显著抗炎镇痛作用具有重要的贡献,将Z-47羰基变成肟或/和将Z-47仲胺基酰化都会造成抗炎镇痛作用的降低甚至是丧失。

Pyridoxine, pyridoxal , pyridoxamine as well as their phosphated forms are structural analogues in which pyridoxal-5"-phosphate and pyridoxamine-5"- phosphate are the biological active forms in vivo which act as the cofactors of aminotransferases, amino acid decarboxylases, cysteine desufbrase and cystathionine , etc by constant transconversions. Recently, it was discovered that B6 played a novel role in tumor growth suppression.

它包括三种结构十分近似的化合物:吡哆醇(Pyidoxine,PN)、吡哆醛(Pyridoxal,PL)和吡哆胺(Pyridoxamine,PM),分别以磷酸化的形式发挥作用,其中吡哆醛-5'-磷酸(Pyridoxal-5'-phosphate,PLP)为B_6在体内的活性形式,通过与磷酸吡哆胺(Pyidoxamine-5-phosphate,PMP)的互变,作为多种酶(氨基转移酶、氨基酸脱羧酶、半胱氨酸脱硫酶、胱硫醚酶等)的辅酶而发挥传递基团的作用。

The results show that HAS has excellent effects of corrosion protection and phosphation acceleration , especially has alkali resistance at a lower temperature.

研究了内含羟胺促进剂的磷化工艺,证明在低温条件下羟胺具有优异的促进作用和耐蚀性,且与氯化钠配合使用可大大降低其有效用量;最后采用正交试验确定最佳磷化配方。

It was found that zymosterol in S. cerevisiae GL7 cells and cycloartenol in P. wickerhamii cells were accumulated when treated with solasodine. Zymosterol and cycloartenol are respective substrates of sterol 24Cmethyltransferase in S. cerevisiae GL7 and P. wickerhamii, hence we deduced that sterol C-24-methyltransferase is the main target of solasodine.

根据澳洲茄胺对S.cerevisiae GL7和P.wickerhamii的甾醇生物合成途径的抑制结果均积累24位甾醇甲基化转移酶的底物,分别是zymosterol和cycloartenol,初步阐明了澳洲茄胺的主要作用靶点是24位甾醇甲基化转移酶,而其它几种抗真菌生药活性成分不影响甾醇的生物合成途径。

Results showed that there were the morphological changes of mitochondria, such as vacuolization, degeneration and cristae swelling or disappearance, in HT-29 cells treated by C2-ceramide for 24 hours. Under the fluorescence microscope, mitochondria of apoptotic cells aggregated and emitted red fluorescence, however, mitochondria of normal cells emitted green fluorescence. The mitochondrial membrane potential began to decrease after 6 hours in HT-29 cells treated with C2-ceramide in time and dose dependent manner.

结果显示C2-神经酰胺作用HT-29细胞24小时,线粒体发生空泡化、变性、嵴肿胀或消失等形态学改变;此时荧光显微镜下可观察到线粒体聚集,发出红色荧光,而正常细胞线粒体发出绿色荧光。C2-神经酰胺作用细胞6小时,线粒体膜电位即开始降低,呈时间-剂量-效应关系。

Two series of polyurethane acrylate grafted acrylic resins (Acr-g-TPU-PETA and Acr-gPPU-PETA) self-emulsifying systems are obtained by grafting -NCO group modified polyurethane acrylates with acrylic copolymer prepared from n-butyl acrylate, styrene,βhydroxyethyl methacrylate and acrylic acid The self-emulsifying systems showed Newtonian fluidity with viscosity closed to that of water, the solid contents were around 30% The T〓 of 15~4℃ for dried film before photocuring favored film formation at room temperature DSC and DMA results showed that PU-PETA is compatible with acrylic resin in the grafted resin The TG and dTG curves for Acr-g-PU-PETA samples were substantially different from the corresponding blends, and the brodened dTG peaks for photocured grafted resin suggest that there might be multiple interactions among chain segments The photocued film of the grafted resins self-emulsifying system exhibited good overall properties with polyurethane acrylate grafts ranging from 30% to 50%, and Acr-g-TPU-PETA series showed better properties than Acr-gPPU-PETA series The adhesion of the photocured film was 1~2 grade, impact strength was 50kg-cm and flexibility was 1mm The Shore hardness and the adhesion of the film decreased markedly if PETA was replaced by HEMA as photoactive group due to the lower C=C double bond content in the grafted resin The polyhydroxy amine-linked thioxanthones photoinitiators can be evenly dispersed in self-emulsifying system without color spot appearing in the dried film The films photocured with IV〓~IV〓 generally exhibited higher Shore hardness, gloss and solventresistance than that cured with Irgacure 2959 and did not induce the rusting of the iron substrate Pigmenting with titanium oxide had no effect on the photocuring The polyhydroxy amine-linked thioxanthone IV〓 and IV〓 can be new candidates for the formulation of titanium oxide pigmented photocurable water-borne coatings for their pale-yellow appearance and slight interference with the color of the coatings WB 4759 with high water-solubility coalesced and separated from the dried resin film, and even induced the rusting of iron substrate.

以丙烯酸丁酯,甲基丙烯酸-β-羟乙酯,丙烯酸及苯乙烯合成厂丙烯酸共聚树脂,并与含-NCO端基的聚氨酯丙烯酸酯接枝反应,经水性化后,得到两个系列(Acr-g-TPU-PETA和Acr-g-PPU-PETA)各5个不同配比的丙烯酸树脂接枝聚氨酯丙烯酸酯自乳化体系,粘度与水相近,为牛顿流体,固含量30%左右。光固化前干燥涂膜的玻璃化转变温度在-15℃~4℃之间,有利于室温下成膜。DSC及DMA谱表明两种树脂基本相容。Acr-g-PU-PETA的热失重行为明显不同于共混材料,接枝样dTG峰明显宽化,表明接枝样中链段之间的相互作刚有多重性,丙烯酸树脂与聚氨酯之间有一定的相容性。接枝树脂自乳化体系光固化涂层的综合性能以聚氨酯丙烯酸酯成分为50%~30%者相对较好,且以Acr-g-TPU-PETA系列更理想。光固化膜的附着力为1~2级,冲击强度为50kg·cm,柔软性多为1mm。以HEMA代替PETA作为接枝树脂的活性基团,碳—碳双键密度太低,光固化膜交联点太少,硬度和附着力均较差。多羟基胺连硫杂蒽酮光引发剂能均匀分散于树脂自乳化体系和接枝树脂干膜中,不出现色斑,光固化膜肖氏硬度一般高于以Irgacure 2959为光引发剂的光固化膜,光泽度及耐丁酮溶剂性能均有所提高,不会诱导铁基生锈,钛白着色对光固化结果几乎没有影响。本论文所合成的多羟基胺连硫杂蒽酮光引发剂IV〓与IV〓为浅黄色,对光固化涂层的颜色干扰较小,为配制钛白着色光固化水性涂料提供了新的光引发剂。水溶性太强的WB 4759在干膜中易聚结析出,且对所附着的铁基有诱导锈蚀作用。

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